Mechanism of analgesic action of mesaconitine. I. Relationship between analgesic effect and central monoamines or opiate receptors

Murayama, Mitsuo; Ito, Tomoko; Konno, Chohachi; Hara, Hiroshi

doi:10.1016/0014-2999(84)90027-x

Cited by 28 publications

(24 citation statements)

References 8 publications

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“…5 Despite these potential side effects, in China BLA in solution (0.2 mg/2 mL; IM) or in tablet (0.4 mg) has been prescribed for the treatment of chronic pain and rheumatoid arthritis. Among many possible in vivo targets, the central catecholaminergic and serotoninergic systems are thought to be involved in analgesia induced by aconitine-like alkaloids 1,6,7. Recently, we reported that BLA when co-injected with lidocaine or epinephrine elicited complete sciatic nerve block that lasted for approximately 4 h in rats 3.…”

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confidence: 99%

Use of Bulleyaconitine A as an Adjuvant for Prolonged Cutaneous Analgesia in the Rat

Wang

Gerner

Schmidt

et al. 2008

Anesthesia &Amp; Analgesia

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BACKGROUND Bulleyaconitine A (BLA) is an analgesic and antiinflammatory drug isolated from Aconitum plants. BLA has several potential targets, including voltage-gated Na+ channels. We tested whether BLA elicited long-lasting cutaneous analgesia, when co-injected with lidocaine and epinephrine, as a model for prolonged infiltration anesthesia. METHODS The local anesthetic properties of BLA were assessed by the patch-clamp technique in HEK293t cells expressing Nav1.7 and Nav1.8 neuronal Na+ channels, both crucial for nociception. Drug solutions (0.6 mL) were injected subcutaneously via rat shaved dorsal skin. Inhibition of the cutaneous trunci muscle reflex was evaluated by pinpricks. Skin cross-sections were stained with hematoxylin and eosin or with antibodies against PGP9.5. RESULTS BLA at 10 µM interacted minimally with resting or inactivated Nav1.7 and Nav1.8 Na+ channels when infrequently stimulated to +50 mV for 3 ms. However, when stimulated at 2 Hz for 1000 pulses, their peak Na+ currents were >90% reduced by BLA. This use-dependent inhibition was not significantly reversed after 15-min washing. Complete nociceptive blockade after injection of lidocaine (0.5%)/epinephrine (1:200,000) lasted for approximately 1 h in rats; full recovery occurred after approximately 6 h. Co-injection of 0.125 mM BLA with lidocaine/epinephrine increased the duration of complete nociceptive blockade to 24 h. Full recovery occurred after approximately 6 days. Skin histology including peripheral nerve fibers appeared unaffected by BLA. CONCLUSIONS BLA inhibits Nav1.7 and Nav1.8 Na+ currents in a use-dependent manner. Co-injection of BLA at ≤0.125 mM with lidocaine and epinephrine elicits complete cutaneous analgesia that lasts for up to 24 h without adverse effects.

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confidence: 99%

Use of Bulleyaconitine A as an Adjuvant for Prolonged Cutaneous Analgesia in the Rat

Wang

Gerner

Schmidt

et al. 2008

Anesthesia &Amp; Analgesia

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“…), inhibited by propranolol i.c.v. and not affected by phenoxybenzamine i.c.v., and that MA increased the turnover rate of noradrenaline in the medulla oblongata as well as pons and spinal cord (Murayama et al, 1984;Murayama & Hikino, 1985). Based on the above evidence, it is postulated that MA antinociception can be elicited via noradrenergic neurones in brain stem and spinal cord.…”

Section: Discussionmentioning

confidence: 95%

“…In this study, MA was now found to cause the antinociceptive effect also in the same sites. However, it is known that the mechanism of the antinociceptive action of MA differs from that of morphine because the antinociceptive effect of MA was not antagonized by levallorphan and the influence of monoaminerelated substances on the antinociception of MA was different from that of morphine (Murayama et al, 1984).…”

Section: Discussionmentioning

confidence: 99%

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Mechanism of the antinociceptive action of mesaconitine: participation of brain stem and lumbar enlargement

Hara

Murayama

1985

British J Pharmacology

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1 The antinociceptive action of mesaconitine (MA) microinjected into the nucleus reticularis gigantocellularis (NRGC), the nucleus reticularis paragigantocellularis (NRPG), the periaqueductal gray (PAG) or the lumbar enlargement was investigated in rats by use of the tail immersion test. In addition, the effects of P-adrenoceptor antagonists and an a-adrenoceptor antagonist administered intrathecally (i.t.) on the antinociceptive action of MA given into the NRPG were also examined by the tail immersion test. 2 MA (50, 100 ng per rat) microinjected into the NRGC, the NRPG, the PAG and the lumbar enlargement increased the response latency in rats in a dose-dependent fashion. MA (50 ng per rat) microinjected into neighbouring sites, the nucleus reticularis parvocellularis, the nucleus originis nervi abducentis and the fasciculus longitudinalis medialis, elicited no significant effect. 5 It is concluded that the NRGC, the NRPG, the PAG and the lumbar enlargement are involved in the sites of the antinociceptive action of MA and that the antinociceptive effect of MA administered into NRPG is elicited by activation of the inhibitory noradrenergic neurones from the NRPG in particularly via P-receptor-mediated effects of noradrenaline.

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“…Aconiti tuber, aconitine and mesaconitine being the main components, has an analgesic action Murayama et al, 1984;Hikino and Murayama, 1985;Isono et al, 1994;Suzuki et al, 1994;Omiya et al, 1999) and a cardiotonic action Kontani and Koshiura, 1983;Perlman and Guideri, 1984;Chen et al, 1990). Aconiti tuber reportedly improves microcirculatory disturbances induced by endotoxin in rats (Zhang et al, 2000).…”

Section: Discussionmentioning

confidence: 97%

Aconiti tuber increases plasma nitrite and nitrate levels in humans

Yamada

Suzuki

Nakaki

et al. 2005

Journal of Ethnopharmacology

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Mechanism of analgesic action of mesaconitine. I. Relationship between analgesic effect and central monoamines or opiate receptors

Cited by 28 publications

References 8 publications

Use of Bulleyaconitine A as an Adjuvant for Prolonged Cutaneous Analgesia in the Rat

Use of Bulleyaconitine A as an Adjuvant for Prolonged Cutaneous Analgesia in the Rat

Mechanism of the antinociceptive action of mesaconitine: participation of brain stem and lumbar enlargement

Aconiti tuber increases plasma nitrite and nitrate levels in humans

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